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Ongiciclib is an orally bioavailable, potent, and highly selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). Developed by Fochon Pharmaceuticals, a subsidiary of Fosun Pharma, the drug is primarily indicated for the treatment of hormone receptor-positive (HR+) and human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Its mechanism involves binding to the ATP-binding site of CDK4 and CDK6, thereby preventing the formation of the CDK4/6-cyclin D complex. This inhibition blocks the phosphorylation of the retinoblastoma (Rb) protein, leading to cell cycle arrest in the G1 phase and suppressing tumor cell proliferation. Ongiciclib is currently undergoing Phase 3 clinical evaluation in combination with endocrine therapies, showing potential as a next-generation CDK4/6 inhibitor with improved selectivity and safety profiles.
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